Transient receptor potential channels: targeting pain at the source

Nat Rev Drug Discov. 2009 Jan;8(1):55-68. doi: 10.1038/nrd2757.


Pain results from the complex processing of neural signals at different levels of the central nervous system, with each signal potentially offering multiple opportunities for pharmacological intervention. A logical strategy for developing novel analgesics is to target the beginning of the pain pathway, and aim potential treatments directly at the nociceptors--the high-threshold primary sensory neurons that detect noxious stimuli. The largest group of receptors that function as noxious stimuli detectors in nociceptors is the transient receptor potential (TRP) channel family. This Review highlights evidence supporting particular TRP channels as targets for analgesics, indicates the likely efficacy profiles of TRP-channel-acting drugs, and discusses the development pathways needed to test candidates as analgesics in humans.

Publication types

  • Review

MeSH terms

  • Analgesics / therapeutic use*
  • Animals
  • Humans
  • Nociceptors / drug effects
  • Nociceptors / physiology*
  • Pain / drug therapy*
  • Pain / etiology
  • Transient Receptor Potential Channels / drug effects
  • Transient Receptor Potential Channels / physiology*


  • Analgesics
  • Transient Receptor Potential Channels